ROCEPHIN (ceftriaxone sodium) FOR INJECTION
HLR 08/25/00
ROCEPHIN (ceftriaxone sodium)
FOR INJECTION DESCRIPTION: Rocephin is a sterile, semisynthetic, broad-spectrum cephalosporin antibiotic for intravenous or intramuscular administration. Ceftriaxone sodium is (6R,7R)-7-[2-(2-Amino-4-thiazolyl)glyoxylamido]-8-oxo-3-[[(1,2,5,6-tetrahydro-2methyl-5,6-dioxo-as-triazin-3-yl)thio]methyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2carboxylic acid, 72-(Z)-(O-methyloxime), disodium salt, sesquaterhydrate. The chemical formula of ceftriaxone sodium is C18H16N8Na2O7S3?3.5H2O. It has a calculated molecular weight of 661.59 and the following structural formula:
Rocephin is a white to yellowish-orange crystalline powder which is readily soluble in water, sparingly soluble in methanol and very slightly soluble in ethanol. The pH of a 1% aqueous solution is approximately 6.7. The color of Rocephin solutions ranges from light yellow to amber, depending on the length of storage, concentration and diluent used. Rocephin contains approximately 83 mg (3.6 mEq) of sodium per gram of ceftriaxone activity. CLINICAL PHARMACOLOGY: Average plasma concentrations of ceftriaxone following a single 30-minute intravenous (IV) infusion of a 0.5, 1 or 2 gm dose and intramuscular (IM) administration of a single 0.5 (250 mg/mL or 350 mg/mL concentrations) or 1 gm dose in healthy subjects are presented in Table 1.
1
HLR 08/25/00
ROCEPHIN (ceftriaxone sodium)
TABLE 1.
Ceftriaxone Plasma Concentrations After Single Dose Administration
Dose/Route
Average Plasma Concentrations (?g/mL)
0.5 hr 1 hr 2 hr 4 hr 6 hr 8 hr 12 hr 16 hr
0.5 gm IV
82 59 48 37 29 23 15 10
0.5 gm IM
250 mg/mL 22 33 38 35 30 26 16 ND
0.5 gm IM
350 mg/mL 20 32 38 34 31 24 16 ND
1 gm IV
151 111 88 67 53 43 28 18
1 gm IM
40 68 76 68 56 44 29 ND
2 gm IV
257 192 154 117 89 74 46 31
IV doses were infused at a constant rate over 30 minutes.
ND = Not determined.
24 hr 5
5
5 9 ND 15
Ceftriaxone was completely absorbed following IM administration with mean maximum plasma concentrations occurring between 2 and 3 hours postdosing. Multiple IV or IM doses ranging from 0.5 to 2 gm at 12- to 24-hour intervals resulted in 15% to 36% accumulation of ceftriaxone above single dose values.
Ceftriaxone concentrations in urine are high, as shown in Table 2.
TABLE 2.
Urinary Concentrations of Ceftriaxone After Single Dose Administration
Dose/Route
0-2 hr
0.5 gm IV
526
0.5 gm IM
115
1 gm IV
995
1 gm IM
504
2 gm IV
2692
ND = Not determined.
Average Urinary Concentrations (?g/mL)
2-4 hr
4-8 hr 8-12 hr 12-24 hr
366
142
87
70
425
308
127
96
855
293
147
132
628
418
237
ND
1976
757
274
198
24-48 hr 15 28 32 ND 40
Thirty-three percent to 67% of a ceftriaxone dose was excreted in the urine as unchanged drug and the remainder was secreted in the bile and ultimately found in the feces as microbiologically inactive compounds. After a 1 gm IV dose, average concentrations of ceftriaxone, determined from 1 to 3 hours after dosing, were 581 ?g/mL in the gallbladder bile, 788 ?g/mL in the common duct bile, 898 ?g/mL in the cystic duct bile, 78.2 ?g/gm in the gallbladder wall and 62.1 ?g/mL in the concurrent plasma.
Over a 0.15 to 3 gm dose range in healthy adult subjects, the values of elimination halflife ranged from 5.8 to 8.7 hours; apparent volume of distribution from 5.78 to 13.5 L; plasma clearance from 0.58 to 1.45 L/hour; and renal clearance from 0.32 to 0.73 L/hour. Ceftriaxone is reversibly bound to human plasma proteins, and the binding decreased from a value of 95% bound at plasma concentrations of ................
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